small molecule inhibitor

CB-6644 is a small molecule inhibitor of the ATPase activity of the RUVBL1 2 complex. It specifically interacts with RUVBL1 2 in cancer cells and blocks the ATPase activity of RUVBL1 2 with a half-maximal inhibitory concentration (IC50) of 15 nM[1].

VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM.

Petesicatib (RG 7625) is a small molecule histone-S (Cat-S) inhibitor for the study of primary dry syndrome and autoimmune diseases.

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

AZD0780 (EX-A6975) is an oral small molecule PCSK9 inhibitor being developed by AstraZeneca as a first-in-class treatment for patients with dyslipidemia that is uncontrolled with statins alone.

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation.

AW68 is a potential small molecule BRD4 inhibitor that prevents and treats BRD4-related diseases and can be used in cancer research.

Casein Kinase II Inhibitor IV is an inducer of epidermal keratinocyte differentiation.

Complement C5-IN-1 is a small-molecule inhibitor of complement component 5 protein (C5).

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

CUR61414 hydrochloride is a potent and cell permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM). CUR61414 hydrochloride is a small-molecule aminoproline class compound. CUR61414 hydrochloride selectively binds to smoothened (Smo, Ki= 44 nM). CUR61414 hydrochloride can induce cancer cells apoptosis without affecting neighboring non-tumor cells.

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

Methotrexate Diglutamate Small molecule compound present in the liver that acts as a partially purified human dihydrofolate reductase inhibitor.

BB-78485 is a potent small molecule inhibitor of LpxC metalloenzymes with antibacterial activity. The IC50 value of BB-78485 against LpxC is 160 nM. BB-78485 can be used for the study of Gram-negative bacterial infections.

Dasantafil (SCH446132) is a small molecule phosphodiesterase-5A (PDE5A) inhibitor used to treat genitourinary disorders and study erectile dysfunction.

Iroxanadine (BRX-005) is a Novel small molecule MAPK p38 inhibitor that induces phosphorylation of p38 SAPK and induces concentration-dependent relaxation in guinea pig pulmonary artery preparations precontracted with phenylephrine.13480-84-5

Isbogrel (CV4151) is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor that can be used to study cardiac arrhythmias, transient ischemic attacks and thrombosis.

Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.Sulmazole has been shown to improve cardiac index, low pulmonary capillary wedge pressure, and can be used in the study of heart failure.Sulmazole is a small molecule cGMP-PDE inhibitor.

WY-47766 (OST-766) is a small molecule proton pump inhibitor that can be used to study postmenopausal osteoporosis.